Depression Treatment Flashcards
What type of family of antidepressants are clomipramine, imipramine, desipramine, amitriptyline, nortriptyline and protriptyline? [1]
TRICYCLIC ANTIDEPRESSANTS (TCAs)
Describe the MoA of TCAs [2]
- Inhibit reuptake of amines on the presynaptic terminal, so 5HT or NA cannot be taken back into neuron
Apart from inhibiting the reuptake of amines, which other receptors do TCAs bind to? [3]
Why is this problematic? [1]
Bind to:
* H1 receptors
* muscarinic receptors
* α1 and α2 adrenoceptors
Causes wide ranging side effects
Look up which TCAs need to know
Important AEs of TCAs? [4]
- Dangerous (cardiotoxic) in overdose
- Anti-cholinergic: dry mouth; blurred vision, constipation, urinary retention, aggravation of narrow angle glaucoma, fatigue, postural hypotension, dizziness, loss of libido, arrhythmias
- Antihistaminic: sedation, weight gain.
- Block alpha 1 adrenoreceptors: orthostatic hypotension - blood pressure drops on standing, cardiac effects
As a result aren’t the first choice!
Phenelzine, tranylcypromine belong to which drug class? [1]
MONOAMINE OXIDASE INHIBITORS
Describe the MoA of monoamine oxidase inhibitors such Phenelzine, tranylcypromine [1]
Which type of food interact with MOIs? [1]
Irreversible inhibition of the enzyme monoamine oxidase [1]
Interactions with tyramine-containing food (mature cheese, pickled fish and meat, red wine, beer, broad bean pods, yeast extract)- restrictions continue at least 2 weeks after discontinuation
Why do you have to wait approx. 2 weeks if you want to change treatment away from MAOIs? [1]
The drugs bind irreversibly: wait for at least 50% of enzymes have been replaced to change treatment
What type of drug class are citalopram, fluoxetine, paroxetine sertraline? [1]
SELECTIVE SEROTONIN REUPTAKE INHIBITORS
What is the benefit of using SSRIs (citalopram, fluoxetine, paroxetine) with regards to AEs [3]
No anticholinergic activity
No cardiotoxic effects
Safe in overdose
Which is the most selective SSRI?
citalopram
sertraline
fluoxetine
paroxetine
Which is the most selective SSRI?
citalopram
sertraline
fluoxetine
paroxetine
AEs of SSRIs?
· Nausea vomiting
· Dry mouth
· Headache
· Asthenia
· Dizziness
· Anorexia
· Weight loss
· Nervousness
· Tremor
· Convulsions
· Sexual dysfunction
Moclobemide belongs to which drug class? [1]
REVERSIBLE MONOAMINE OXIDASE INHIBITOR
What are the different targets for reverible MAOIs compared to irreversible MOAIs? [2]
Describe the benefits of reversible MAOIs compared to irreversible MAOs [2]
Drug targets:
* Reversible MAOI targets: MOA-A
* Irreversible MAOI targets: MAOA versus MAOB
Differences:
* Reversible is safer than irreversible MAOIs
* Can switch drug classes quicker
Which is the safest monoamine oxidisase inhibitor?
Moclobemide
Phenelzine
Tranylcypromine
Which is the safest monoamine oxidisase inhibitor?
Moclobemide (reversible MOAIs)
Phenelzine (irreversible MOAIs)
Tranylcypromine (irreversible MOAIs)
Describe MoA of Agomelatine [2]
Why is this potentially a really good drug? [2]
MoA:
* Agonist at melatonin MT1 & MT2 receptors: important for sleep control
* Antagonist of 5-HT2 receptors
Benefits of Agomelatine:
* improves sleep quality
* less sexual dysfunction than SSRIs;
* anxiolytic effects
* no ‘discontinuation syndrome’
The treatment with the SNRI [] reduces the increased Default Mode Network
connectivity seen in depression
The treatment with the SNRI duloxetine reduces the increased Default Mode Network connectivity seen in depression
How long do antidepressant drugs take to cause action in the body?
Although the level of drug increases in plasma soon after the patient starts taking the medication, there is a delayed onset of action of 1-2 weeks
Explain why there is a delayed action for anti-depressant drug action for TCAs [4]
The immediate increase in synaptic concentration of amines
may lead to activation of somatic neuronal autoreceptors
The activated autoreceptors decrease firing of the neurones
During the first weeks of treatment the autoreceptors desensitize
The neurones will return subsequently to the normal firing rate
The inhibition of reuptake continues and the level of amines
continues to be high, resulting in full efficacy
Explain the three phases of antidepressant treatment [3]
Acute Treatment
- First 6-12 weeks of treatment; aims at remission (control of symptoms)
- Inadequate early response is associated with poor prognosis
Continuation Treatment
- for 6 months after full symptom control; to maintain remission status and prevent relapse
Maintenance Treatment
- Aims at prevention of recurrence of a further episode of depression.
- Indicated when higher risk of these recurrence; “maintenance dose”.
Which of the following class of drug causes this symptom?
TCAs
SNRIs
MAOIs
SSRIs
(orthostatic hypotension)
Which of the following class of drug causes this symptom?
TCAs: due to blocking of Block alpha 1 adrenoreceptors
SNRIs
MAOIs
SSRIs
